Bazedoxifene: a novel selective estrogen receptor modulator for postmenopausal osteoporosis.

Abstract

Several new selective estrogen receptor modulators (SERMs) are currently under clinical development for the prevention and/or treatment of postmenopausal osteoporosis, with the goal of optimizing the estrogen receptor agonist/antagonist activity in target tissues. Bazedoxifene is a novel SERM under clinical investigation for the prevention and treatment of postmenopausal osteoporosis. Emerging clinical data have shown that bazedoxifene is effective in preventing bone loss and osteoporotic fractures in postmenopausal women, with no evidence of breast or endometrial stimulation. Two large, prospective, international phase 3 studies have been completed. In postmenopausal women at risk for osteoporosis, bazedoxifene has been shown to preserve bone mineral density and to reduce bone turnover. In postmenopausal women with osteoporosis, bazedoxifene has demonstrated significant protection against new vertebral fractures and against non-vertebral fractures in women at higher fracture risk. The treatment effects of bazedoxifene were supported by findings from independent re-analyses using the Fracture Risk Assessment Tool (FRAX), which showed that bazedoxifene significantly reduced the risk of all clinical and morphometric vertebral fracture and of non-vertebral fracture in women at or above a FRAX-based threshold. Bazedoxifene was generally safe and well tolerated in the phase 3 studies and showed neutral effects on the breast and an excellent endometrial safety profile; such attributes allow for the partnering of bazedoxifene with conjugated estrogens for menopausal symptom relief. Collectively, these results suggest that bazedoxifene may be a promising new therapy for the prevention and treatment of postmenopausal osteoporosis as a monotherapy or in combination with conjugated estrogens in menopausal hormone therapy.

• Authors: T J de Villiers
• Journal: Climacteric : the journal of the International Menopause Society (Climacteric) Vol. 13 Issue 3 Pg. 210-8 (Jun 2010) ISSN: 1473-0804 [Electronic] England
• PMID: 20184423 (Publication Type: Journal Article, Review)

Chemical References

• Indoles
• Lipids
• Selective Estrogen Receptor Modulators
• bazedoxifene

Topics

• Clinical Trials, Phase III as Topic
• Endometrium (diagnostic imaging)
• Female
• Fractures, Bone (etiology, prevention & control)
• Humans
• Indoles (therapeutic use)
• Lipids (blood)
• Mammography
• Osteoporosis, Postmenopausal (complications, drug therapy)
• Selective Estrogen Receptor Modulators (therapeutic use)
• Ultrasonography
• Venous Thromboembolism (epidemiology)